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Chiral Phosphoric Acid-Catalyzed Enantioselective Construction of 2,3-Disubstituted Indolines

Wei‐Yang Ma, Coralie Gelis, Damien Bouchet, Pascal Retailleau, Xavier Moreau, Luc Neuville, Géraldine Masson

2021Organic Letters32 citationsDOIOpen Access PDF

Abstract

Highly enantio- and regioselective (3 + 2) formal cycloaddition of β-substituted ene- and thioenecarbamates as well as cyclic enamides with quinone diimides catalyzed by a BINOL- and SPINOL-derived phosphoric acid is reported. A wide variety of 2,3-disubstituted 2-aminoindolines, including polycyclic ones, were prepared in generally high yields (up to 98%) with moderate to complete diastereoselectivities and in most cases excellent enantioselectivities (up to 99% ee).

Topics & Concepts

ChemistryPhosphoric acidRegioselectivityEnantioselective synthesisCycloadditionCatalysisCombinatorial chemistryOrganic chemistryAsymmetric Synthesis and CatalysisSynthesis and Catalytic ReactionsOxidative Organic Chemistry Reactions
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